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Pharmaceutical Compositions Containing Diacerein

a technology of diacerein and composition, applied in the field of diacerein-containing pharmaceutical compositions, can solve problems such as local effects in the colon, and achieve the effects of reducing adverse side effects of diarrhea, and increasing bioavailability

Inactive Publication Date: 2010-04-29
TWI BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0006]An object of the present invention is to provide a once-daily controlled-release formulation of diacerein for treating inflammatory, autoimmune diseases or their complications, such as osteoarthritis, type I / II diabetes or diabetic nephropathy, with reduced adverse side effects. More specifically, the once-daily controlled-release formulations of diacerein of the present invention could be a membrane-controlled formulation, a matrix formulation or an osmotic pump formulation. In a preferred embodiment, the controlled-release formulations of diacerein of the present invention could further provide increased bioavailability when compared to commercial immediate release (IR) formulations. More specifically, said method reduces the adverse side effect of diarrhea caused by diacerein.

Problems solved by technology

Even though feeding increases the bioavailability of diacerein to 43˜70%, incomplete absorption still results in a local effect in the colon.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

Preparation of Solid Dispersion

[0049]Acceptable ranges for the components of representative solid dispersions are shown in Table 3.

TABLE 3IngredientsExamples%APIDiacerein10~90Carriershydrophilic polymers (HPMC, HPC, HEC, MC, sod. CMC etc.),10~90hydrophobic polymers (EC, PVA, Methylmethacrylate etc.),Surfactants (SLS, Tween 80, Gelucire, Cremophor,poloxamer, PEG etc.),water-soluble excipients (lactose, sucrose, mannitol,glucose etc.),Wax (glyceryl behenate, cetyl alcohol etc.), orcombinations thereofOrganic solventsAcetone, Isopropyl alcohol, or Ethanolqs

Process:

[0050]Diacerein may be dissolved with suitable organic solvents to form a drug solution. Carriers, such as hydrophilic polymers, hydrophobic polymers, surfactants, water-soluble excipients, or wax, or a combination of the above carriers are then dissolved or dispersed in the drug solution. Spray drying of the above solution may be used to obtain a solid dispersion, or the solution may be coated onto suitable excipients (water...

example 2

Complexation with Cyclodextrins

[0051]Acceptable ranges for the components of representative complexes with cyclodextrins are shown in Table 4.

TABLE 4Ingredients%APIDiacerein10~90Cyclodextrinsα-cyclodextrin, β-cyclodextrin,10~90γ-cyclodextrin and their derivatives, forexample, 2-hydroxypropyl-β-cyclodextrin etc.

Process:

[0052]Water solutions of cyclodextrins may be prepared with various percentages. Diacerein is added to the above solutions to yield saturated solutions. The solutions are stirred for at least 72 hours and then allowed to stand until all undissolved material has precipitated. The supernatant solution is filtered and dried by oven, spray drying or freeze drying or coated onto suitable excipients (which function as diluents) using a fluidized bed.

example 3

Matrix System (Tablet)

[0053]Acceptable ranges for the components of representative tablet matrix systems are shown in Table 5.

TABLE 5Ingredients%APIDiacerein, Diacerein in solid dispersion or in comlexation with10~90cyclodextrinsControlledwater-swellable polymers, hydrophilic polymers (HPMC,10~90releaseHPC, HEC, MC, sod. CMC etc.), hydrophobic polymersmaterials(EC, PVA, Methylmethacrylate etc.), wax (glycerylbehenate, cetyl alcohol etc.).

Process:

[0054]The API part is prepared as described in the above examples. The diacerein API part is physically mixed or granulated with controlled release materials and then the mixture is compressed to obtain matrix tablets. Optionally, an acidifying agent or buffering agent may be included in the tablet formulation.

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PUM

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Abstract

A once-daily controlled-release formulation of diacerein for treating inflammatory or autoimmune diseases or their complications, with reduced adverse side effects and methods of treating such diseases are disclosed.

Description

BACKGROUND OF THE INVENTION[0001]Diacerein (4,5-bis(acetyloxy)-9,10-dioxo-2-anthracene carboxylic acid) is a highly purified anthraquinone derivative. It is known to inhibit interleukin-1 activity, and has been approved as a Symptomatic Slow-Acting Drug in Osteoarthritis (SYSADOA) in several countries.[0002]Diacerein has a log P value of 2.42 and is practically insoluble in water. Diacerein is entirely converted into rhein before reaching the systemic circulation. Rhein itself is either eliminated by the renal route (20%) or conjugated in the liver to rhein glucuronide (60%) and rhein sulfate (20%). These metabolites are mainly eliminated by the kidney.[0003]There are two major adverse side effects of diacerein: diarrhea or soft stools and yellow-brown coloring of urine. The severity of diarrhea is mild-to-moderate and occurs within the first two weeks of treatment. Coloring of urine is due to the metabolites of diacerein present in the urine. In vitro and in vivo studies have showe...

Claims

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Application Information

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IPC IPC(8): A61K31/225A61K9/14A61P29/00A61P3/10A61P19/10A61P25/00
CPCA61K9/146A61K9/1676A61K9/2013A61K9/2018A61K9/2054A61K31/235A61K9/2846A61K9/2853A61K9/2866A61K9/5078A61K9/284A61K47/6951A61P1/02A61P1/04A61P11/00A61P11/06A61P13/12A61P17/00A61P17/02A61P17/06A61P19/00A61P19/02A61P19/10A61P25/00A61P29/00A61P37/00A61P37/02A61P37/06A61P37/08A61P43/00A61P9/10A61P3/10
Inventor GAO, DANCHENWU, JEN-SENLU, WEI-SHUCHEN, SHOUCHIUNGKUO, PEI-CHUNCHEN, CHIH-MING
Owner TWI BIOTECH
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